The invention relates to dermatological agents containing fruit extracts and methods of using the same to treat dermatological disorders. In particular, the fruit extracts include extracts from apricots, apples, peaches, pears, pineapples, papayas, pomegranates, cherries, kiwis, tangerines, grapes, and oranges.
The skin is the most environmentally-stressed organ in mammals, particularly in humans. Not only is the skin subjected to toxic chemicals and hostile environments, but it is also the only organ directly exposed to ultraviolet (xe2x80x9cUVxe2x80x9d) light in the presence of oxygen. [See, e.g., P. Mayer, et al., Cosmetic and Toiletries, 108:99-109 (February 1993)]. Lengthy exposure of the skin to UV light typically damages the skin, resulting in sunburn, photoaging and carcinogenesis.
UV light exposure in the presence of oxygen results in the creation of free radicals. In the skin, these radicals frequently trigger the release of inflammatory mediators, commonly manifested as sun burn; cytoskeletal alterations, breaking down the collagen in the skin; and may also result in structural DNA changes, such as DNA strand breaks and dimer formation. [K. Werninghaus, et al., Arch Dermatol., 130:1257-1261 (October 1994)]. The body attempts to neutralize the free radicals generated by UV light through the use of antioxidants. Antioxidants are commonly found in two forms: enzymatic and non-enzymatic. Superoxide dismutase (SOD), catalase, and glutathione peroxidase are some of the natural enzymatic antioxidants used by the body. SOD accelerates the spontaneous reduction of superoxide free radicals into peroxides and oxygen. Catalase then further decomposes hydrogen peroxide into water and oxygen. Finally, the glutathione peroxidase reduces both hydrogen peroxide and free organic hydroperoxides. Some non-enzymatic antioxidants, such as Vitamin E (tocopherol), Vitanin A (beta-carotene), and Vitamin C (ascorbic acid) have each been individually applied to assist the skin in scavenging free radicals and neutralizing the harmful effects of UV light. [P. Pugliese, xe2x80x9cA Brief Introduction to Free Radicals and Oxygen Stress,xe2x80x9d Paper presented at International Conference of Aesthetics and Dermatology, Los Angeles, (February 1991)]. Conventional skin protection efforts typically attempt to either shield the skin from UV light to prevent the production of free radicals or provide additional agents capable of neutralizing the free radicals.
Topical applications are one such effort known in the art to help shield the skin from the sun""s harmful UV effects. These sun-screens often are water- or oil-based lotions or ointments that incorporate photo-protectant materials such as titanium and zinc oxide. [J. Weiss, Skin, 16-23 (March/April 1996)]. Although the most widely used form of protection against exposure to sunlight, these topical applications tend to suffer from several drawbacks. First, large amounts of photo-protective materials are usually incorporated into the topical applications, some of which have recently become suspected of having toxicity or otherwise being harmful under these conditions. Furthermore, the effectiveness of such topical applications is dependent upon a constant and uniform coverage of the skin, which is often difficult to obtain. Many individuals fail to use these topical sunscreens on a regular or continuing basis, as is required under prolonged UV exposure. Finally, sunscreens and other topical applications do not consistently provide good protection for all types of UV light. [Id.].
It is also known that certain fruit extracts may be added to preparations, such as lotions, creams and gels, which are topically applied to the skin, usually for fragrance or conditioning, i.e., softening the skin.
F-D-C Accession No. 02150070012, The Rose Sheet, Feb. 14, 1994, Vol. 15, Issue 7 discloses a skin lotion and cream that combines the benefits of alpha hydroxy acid, antioxidants and sunscreen in one product. The composition is formulated with green tea extract and a triple fruit acid complex to allegedly smooth skin texture, reduce the appearance of fine wrinkles and lines and even out skin tone. The composition also contains a combination of melanin and vitamin E that allegedly neutralizes free radicals before they can damage the skin and an SPF 8 broad spectrum sunscreen.
F-D-C Accession No. 02150250004, The Rose Sheet, Jun. 20, 1994, Vol. 15, Issue 25 discloses a passion flower shower and bath gel that has a fruity fragrance and contains passion flower and extracts of orange flower, mango, strawberry, grapefruit and lavender. Also disclosed is a Vitamin E flower shower and bath gel formula with a light floral fragrance that includes the antioxidant Vitamin E, as well as ginseng, elder flower and rosemary extracts, apricot oil and lavender.
F-D-C Accession No. 02160380003, The Rose Sheet, Sep. 18, 1995, Vol. 16, Issue 38 discloses a triple action complex containing apple extract that allegedly inhibits the effects of irritants and makes skin more resilient, kola nut extract that allegedly defuses the irritation potential of skin-damaging free radicals, bisabool to soothe, and an unspecified antioxidant complex.
F-D-C Accession No. 02170140007, The Rose Sheet, Apr. 1, 1996, Vol. 17, Issue 14 discloses a self tanner formulated with alpha- and beta-hydroxy acids, as well as phytoglycolipids to extend color and prevent skin peeling, an Environmental Protection Complex to neutralize free radicals, and apple extract to help firm skin. The Environmental Protection Complex contains green tea, co-enzyme Q-10 and Vitamins E and C.
F-D-C Accession No. 02170370002, The Rose Sheet, Sep. 19, 1996, Vol. 17, Issue 37 discloses bath and shower gels and body lotions available in pear, pink grapefruit, pomegranate and tangerine fragrances. Also disclosed are body lotions having kiwi fruit, orange peel, apricot, and Vitamin E and provitamins B5 to allegedly help condition skin.
F-D-C Accession No. 02170440013, The Rose Sheet, Oct. 28, 1996, Vol. 17, Issue 44 discloses a pink grapefruit facial soap with grapefruit seed, orange blossom and yarrow extracts that leaves behind a soft, smooth moisturized complexion.
F-D-C Accession No. 02170440015, The Rose Sheet, Oct. 28, 1996, Volume 17, Issue 44 discloses a body wash formulated with seaweed, orange peel extract and sage extract that leaves the skin hydrated and revitalized. Also disclosed is a hand cream containing seaweed, green tea extract, cooling eucalyptus, and shea butter.
F-D-C Accession No. 02170500003, The Rose Sheet, Dec. 9, 1996, Vol. 17, Issue 50 discloses a scent named Green Tea eau de toilette, which has notes of freesia, green pineapple, Granny Smith apple, along with Japanese green tea, pink grapefruit, bergamont, mandarin and mint accords.
F-D-C Accession No. 02180100000, The Rose Sheet, Mar. 10, 1997, Vol. 18, Issue 10 discloses a lotion for face and throat that allegedly provides the immediate perception of firm, uplifted skin using a ceramide retinyl complex, which combines the xe2x80x9canti-aging propertiesxe2x80x9d of ceramide 6 and retinyl linoleate with the tissue respiratory factors found in Vitamin C and apple extract.
F-D-C Accession No. 05050320012, The Tan Sheet, Aug. 11, 1997, Vol. 5, Issue 32 discloses a Fruit Polyphenol Antioxidant Complex xe2x80x9cVegicapxe2x80x9d with extracts from cherries, apples, apricots, prunes, pomegranates, quercetin, and vitamin C. Also disclosed is a formulation including hawthorne berry extract.
F-D-C Accession No. 0219008005, The Rose Sheet, Feb. 23, 1998, Vol. 19, Issue 8 discloses a body lotion moisturizer that combines BHAs, AHAs, vitamins A, E and green tea extract to exfoliate skin while providing antioxidant benefits. Other antioxidants contained in the product include willow, apple and lemon extract blend,
F-D-C Accession No. 02190130012, The Rose Sheet, Mar. 30, 1998, Vol. 19, Issue 13 discloses a Daily Moisture Care cream-gel that pairs Calabria orange extract with antioxidants to allegedly strengthen the skin""s natural defense system while keeping skin healthy and supple.
U.S. Pat. No. 4,857,325 to Albeck et al. discloses antioxidant compositions and methods for enhancing the texture of the skin, which compositions are prepared by the water extraction of natural antioxidants from plant substrates. The plant tissues from which these water soluble antioxidants may be obtained are the leaves of spinach, clover, alfalfa, corn, tobacco, onion, garlic and algae. Other suitable plants may also be utilized if the extract of green leaves provides an antioxidant effect. The antioxidant may be used in a variety of cosmetics and is alleged to have a protective effect against ultraviolet light damage to the skin. Therefore, the antioxidant may be applied to the skin to prevent damage caused by radiation from natural sources such as the sun, or from artificial sources, either alone or in combination with other sunscreen agents.
U.S. Pat. No. 4,923,697 to Albeck et al. similarly discloses a water soluble antioxidant obtained from plants of the order Chenopodiales which has the capability of lowering the peroxide level of the skin. The antioxidant is obtained by extraction of the plant tissue with water and thereafter chromatographically separating the antioxidant component.
U.S. Pat. No. 5,124,167 to Albeck et al. similarly discloses such cosmetic compositions including a cosmetically acceptable carrier and an effective amount of a water soluble antioxidants, derived from plant tissues, which is capable of being absorbed into mammalian skin to reduce the peroxide level.
U.S. Pat. No. 5,204,105 to Mausner discloses an emulsified cosmetic composition which reduces puffy skin and dark circles under the eyes, making the contour of the skin smoother, and for reducing sensations of irritation and inflammation of the skin under the eyes. The composition is selected from the group consisting of plant extracts, yeast extracts, and a combination thereof. The plant extracts include butcher broom, hydrocotyl, horse chestnut, calendula, hamamelis, horsetail, euphrasia, peach, lady""s mantle, ivy, chamomile matricaria and comfrey.
U.S. Pat. No. 5,441,740 to Ozlen discloses a cosmetic composition containing at least one alpha-hydroxy acid, salicylic acid and at least one digestive enzyme derived from fruit. Preferably the digestive enzyme is a mixture of bromelain and papain. Bromelain is disclosed as being typically obtained from pineapples and papain is disclosed as being typically obtained from dry papaya latex. The compositions are allegedly useful for treating various cosmetic conditions or dermatological disorders, such as lack of adequate skin firmness, wrinkles, and dry skin.
U.S. Pat. No. 5,587,174 to Lang et al. discloses a skin and hair treatment composition that includes apple wax, as well as methods for obtaining such compositions. The apple wax is obtained by extraction of depectinized apple pomace with a variety of solvents and evaporation of the extract. The apple wax is generally disclosed to have a protective effect on the skin. Compositions according to the invention can take the form of a variety of preparations for the care or protection of skin.
U.S. Pat. No. 5,824,320 to Rouillard et al. discloses a cosmetic or pharmaceutical composition containing mangiferine, or derivatives thereof, of natural origin or obtained by chemical, enzymatic or biological synthesis, as well as compositions containing a mangiferine plant extract, in particular an Apholia or Mangifera leaf extract. Mangiferine and its derivatives, in purified form or contained in plant extracts, possess high anti-ultraviolet, anti-collagenase and anti-elastic activity. Thus, they are alleged to be particularly useful in cosmetic or pharmaceutical compositions intended for the protection of the epidermis against ultraviolet rays, for enhancing the structural quality of the skin and for providing help in combating biological and/or actinic skin aging.
U.S. Pat. No. 5,891,440 to Lansky discloses a phytoestrogen supplement prepared from pomegranate seeds and a method of preparing the supplement. The supplement can be administered orally or topically. The oral phytoestrogen supplement includes a pomegranate extract, prepared by contacting pomegranate seeds with an appropriate solvent that is non-toxic for oral use, and an aqueous extract prepared by contacting water with an herbal mixture that includes schizandra berries and Chinese asparagus root. The topical supplement includes pomegranate oil obtained from pressed pomegranate seeds and coconut milk.
U.S. Pat. No. 5,073,545 to Arima et al. discloses a method for lightening and whitening skin that comprises externally applying a composition including one or more ellagic acid compounds.
U.S. Pat. No. 5,141,741 to Ishida et al. discloses an anti-sunburn skin care composition containing a polyvalent metal salt of an ellagic acid compound and a cosmetic carrier, as well as a method of protecting human skin from sunburn by applying the composition to the human skin.
In addition, various conventional supplements have attempted to boost the body""s natural antioxidant activity using vitamins, minerals, and herbs. Vitamin C, for example, is believed to reduce sun damage, and vitamin E has been used topically as an anti-inflammatory agent and for UV-ray protection of cells. Also, carotenoids may have usefulness as antioxidants, protecting against both free radicals and singlet oxygen, a highly reactive, diamagnetic excited state of dioxygen. Moreover, it is thought that minerals are typically needed to maintain the effectiveness of the body""s enzymatic antioxidants. Both copper and zinc are thought to be necessary in the proper functioning of SOD. [G. La Ruche and J.-P. Cesarini, Photodermatol Photoimmunol Photomed., 8:232-235 (1991)]. Manganese is believed to be a cofactor in the mitochondrial form of SOD. Also, selenium is thought to be necessary for glutathione peroxidase activity, one of the enzymatic antioxidants found naturally in the body. Unfortunately, few experiments into the skin-protecting effects of these antioxidants have provided scientific or conclusive results.
In particular, a study that orally administered vitamin E supplements to participants and then tested their response to the sun found that Vitamin E did not mitigate the UV damage, despite the fact that the subjects were given thirteen times the recommended daily allowance. [K. Werninghaus, et al., Arch. Dermatol., 130:1257-1261 (October 1994)]. Furthermore, beta-carotene has been reported to have beneficial effects in some studies, but has had no effect in others. Finally, another study noted the photo-protective effect of the oral administration of butylated hydroxy toluene, but little effect was shown using vitamins C or E.
Certain herbs have also been found helpful in protecting the skin from the sun""s harmful effects. Herb extracts such as burdock root, echinacea, yellow dock root and grape seeds posses detoxifying properties that have been individually applied to help the body eliminate harmful free radicals. Burdock root contains the active ingredient inulin, and is useful in treating cancerous skin conditions, as well as inflammation. Echinacoside and caffeoyl derivatives present in echinacea act as antioxidants, which protect the skin when applied topically. [R. Facino, et al., Planta Med. 61:510-514 (1995)]. Yellow dock root contains the active constituent chrysarobin, which has been used in the treatment of chronic skin diseases, such as eczema, leprosy, psoriasis, and cancer. [M. Tierra, xe2x80x9cPlanetary Herbology,xe2x80x9d p. 194 (1988)]. Potent bioflavanoids, known as oligomeric proanthocyanidins (OPC""s), are found in grape seeds. These OPC""s are thought to be potent antioxidants possessing 20 times the antioxidant power of vitamin C and 50 times the antioxidant power of vitamin E. These herbs have been individually used both topically and orally to protect the skin from various afflictions.
Other studies have attempted to demonstrate the synergistic effect of a mixture of antioxidants. In one study, the subjects were given selenium and copper along with a vitamin supplement of vitamin A and E. [G. La Ruche and J. P. Cesarini, Photodermatol Photoimmunol Photomed., 8:232-235 (1991)]. Although the supplements did protect the skin cells to some extent against ultraviolet-induced cell damage, they did not prevent light-induced erythema, i.e., redness.
Also, U.S. Pat. No. 5,290,605, discloses a soft drink that provides protection against sun damage. This drink contains a mixture of carotenoids, optionally together with vitamin C, vitamin E, or other effective antioxidants. The above antioxidants are limited to an amount which does not exceed ten vitamin ARDA equivalents of provitamin A per liter of drink.
Nutritional supplements such as Source Naturals"" PYCNOGENOL(copyright) COMPLEX(trademark) provide a variety of vitamins, minerals and herb extracts to allegedly protect the body against free radicals. In particular, the PYCNOGENOL(copyright) COMPLEX(trademark) contains pycnogenol, proanthodyn, quercetin, Ginkgo Biloba extract, Green Tea extract, Bilberry extract, Silymarin, Tumeric extract, Hawthorn Berry extract, Rosemary extract, vitamin C (in the form of zinc and magnesium ascorbates), and magnesium.
Also, an herbal supplement and nutritional suggestions for the maintenance of the skin are disclosed in xe2x80x9cThe Scientific Validation of Herbal Medicinexe2x80x9d by Daniel B. Mowrey, Ph. D. (p.247-251 1986). The herbal supplement consists of extracts of chaparral, dandelion root, burdock root, licorice root, echinacea, yellow dock root, kelp and cayenne. The reference also suggests the use of the following nutritional supplements: vitamin A, vitamin B1, vitamin B2, vitamin B6, a vitamin B complex, vitamin C, vitamin D, vitamin E, niacinamide, pantothenic acid, para-aminobenzoic acid, biotin, choline, inositol, folic acid, zinc, calcium, magnesium, and potassium.
Fruits, vegetables, and commonly used spice and herbs have also been stated to contain cancer protective factors [L. Dragsted, M. Strube, and J. C. Larsen, Pharmacology and Toxicology, v. 72, S1, pp. S116-S135 (1993)].
Although the above references disclose various supplements for the skin and studies concerning these supplements, there is no disclosure or suggestion of dermatological agents containing fruit extracts from apricots, apples, peaches, pears, pineapples, papayas, pomegranates, cherries, kiwis, tangerines, grapes, and oranges and methods of employing one or more of such fruit extracts for managing dermatological conditions.
The invention relates to compositions for managing dermatological conditions that contain at least one fruit extract from pomegranate in an amount sufficient to neutralize free radicals, a moisturizing agent in an amount sufficient to facilitate hydration of the skin, and a pharmaceutically acceptable carrier. The fruit extract may be present in an amount from about 0.01 to 80 weight percent.
The moisturizing agent may be a mono- or poly-hydroxy acids, a hydrophobic agents, a hydrophilic agents, or a mixture thereof. The mono- or poly-hydroxy acid may be glycolic acid, lactic acid, citric acid, tannic acid, salicylic acid, or a mixture thereof. The hydrophobic agent may be seramide, borage oil, tocopherol linoleate, dimethicone, glycerine, or a mixture thereof. The hydrophilic agent may be hyaluronic acid, sodium peroxylinecarbolic acid, wheat protein, hair keratin amino acids, or a mixture thereof. Other moisturizing agents include primrose oil, GLA 3, flax seed oil, and mixtures thereof.
The dermatological agent may also include at least one sunscreen or sunblock component such as titanium dioxide, zinc oxide, talc, red veterinary petrolatum, a cinnamate, a benzone, a salicylate, a benzoic acid, a benzophenone, or mixtures thereof.
The dermatological agent may also include at least one cysteine component, magnesium component, manganese component, copper component, or selenium component. The cysteine component, if present, may be N-acetyl cysteine and may be present in an amount from about 1 to 10 weight percent; the magnesium component, if present, may be magnesium ascorbate and may be present in an amount from about 1 to 10 weight percent, wherein the magnesium is present in an amount from about 10 to 30 weight percent of the complex; the manganese component, if present, may be manganese ascorbate and may be present in an amount from about 0.5 to 10 weight percent, wherein manganese is present in an amount from about 5 to 20 weight percent of the complex; or the copper component, if present may be copper sebacate and may be present in an amount from about 0.01 to 5 weight percent, wherein the copper is present in an amount from about 5 to 20 weight percent of the complex.
The dermatological agent may also include at least one of wild yam root, wild yam extract, yellow dock, bupleurum, poria cocos, gentian root, myrrh gum, hawthorn berry extract, marshmallow root, rosemary extract, black cohosh, soy, and ginger. The amount of wild yam root, wild yam extract, marshmallow root, hawthorn berry extract, and rosemary extract, if present, may be from about 0.5 to 8 weight percent each; the amount of yellow dock, if present, may be from about 1 to 30 weight percent; and the amount of bupleurum, poria cocos, gentian root and myrrh gum, if present, may be from about 1 to 20 weight percent each.
The dermatological agent may also include at least one anti-inflammatory component in an amount sufficient to reduce inflammation of the patient""s skin, at least one immunity boosting component in an amount sufficient to stimulate the patient""s immune system response to prevent or facilitate repair of damaged skin, or an antioxidant. The anti-inflammatory component may be present in an amount from about 5 to 40 weight percent and may be a vitamin E source, a transition metal component, aloe vera gel, aloe vera, licorice extract, pilewort, Canadian willow root, zinc, allantoin, or a mixture thereof. The immunity boosting component may be present in an amount from about 1 to 20 weight percent and may be echinacea, echinacea extract, golden seal, or a mixture thereof. The antioxidant may be a catechin-based preparation, a vitamin A source, a ginko biloba extract, a silymarin source, a quercetin compound, a vitamin C source, a carotenoid, or mixtures thereof. The dermatological agent may be adapted for oral administration or topical administration.
Another embodiment of the invention relates to a dermatological agent for managing a dermatological condition in a patient having skin containing at least one fruit extract in an amount sufficient to neutralize free radicals, a transition metal component in an amount sufficient to inhibit or reduce inflammation, and a pharmaceutically acceptable carrier. The fruit extract can be an extract from apricots, apples, pears, peaches, pineapples, papayas, pomegranates, cherries, kiwis, tangerines, grapes, oranges, or a mixture thereof. In a preferred embodiment the extract is an extract from pears, peaches, pineapples, papayas, pomegranates, kiwis, tangerines, oranges, or a mixture thereof. The transition metal component may be zinc.